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Assay Detail

CHEMBL3271121

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of BuChE in human serum using S-butyrylthiocholine iodide as substrate preincubated with enzyme for 20 mins followed by substrate addition by Ellman's method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Serum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cholinesterase (CHEMBL1914)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of benzylisoquinoline derivatives as multifunctional agents against Alzheimer's disease.
Xu ZC, Wang XB, Yu WY, Xie SS, Li SY, Kong LY.
Bioorg Med Chem Lett (2014) 24 : 2368 -2373
PubMed 24726809 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.02 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3262667 1 5.64
CHEMBL3262666 1 5.49
CHEMBL3262661 1 5.46
CHEMBL3262665 1 5.23
CHEMBL3262663 1 5.22
CHEMBL3262664 1 5.19
CHEMBL3262673 1 5.03
CHEMBL3262669 1 4.97
CHEMBL3262662 1 4.95
CHEMBL3262671 1 4.89
CHEMBL3262670 1 4.80
CHEMBL3262658 1 4.78
CHEMBL3262672 1 4.66
CHEMBL3262668 1 4.62
CHEMBL510363 1 4.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3262667 IC50 = 2270.0 nM 5.64
CHEMBL3262666 IC50 = 3250.0 nM 5.49
CHEMBL3262661 IC50 = 3430.0 nM 5.46
CHEMBL3262665 IC50 = 5830.0 nM 5.23
CHEMBL3262663 IC50 = 6020.0 nM 5.22
CHEMBL3262664 IC50 = 6420.0 nM 5.19
CHEMBL3262673 IC50 = 9290.0 nM 5.03
CHEMBL3262669 IC50 = 10590.0 nM 4.97
CHEMBL3262662 IC50 = 11170.0 nM 4.95
CHEMBL3262671 IC50 = 12900.0 nM 4.89
CHEMBL3262670 IC50 = 15900.0 nM 4.80
CHEMBL3262658 IC50 = 16700.0 nM 4.78
CHEMBL3262672 IC50 = 21710.0 nM 4.66
CHEMBL3262668 IC50 = 23730.0 nM 4.62
CHEMBL510363 IC50 = 46770.0 nM 4.33